|4-(4-(苯并[d][1,3]二恶茂-5-基)-5-(吡啶-2-基)-1H-咪唑-2-基)苯甲酰胺|CsnPharm

CAS No.: 301836-41-9

SB 431542 Catalog No. CSN11900

Synonyms: SB-431542

SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold selective for ALK5 than p38 MAPK and other kinases.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The TGF-β pathway regulates a wide variety of cellular processes in many different cell types and biological contexts. There are three identified TGF receptor ligands, TGF-β1, 2 and 3. Activated TGF-β ligands can interact with TGF-β type II receptors (TβRII), then recruit and phosphorylate the TGF-β type I receptors (also called as TβRI or ALK5). In turn, activated TβRI phosphorylates SMAD2 and SMAD3 at C-terminal serine residues. Following that, phosphorylated SMAD and SMAD3 assemble into heterodimeric and trimeric complexes with SMAD4. Then the trimeric complex translocate into the nucleus and regulate the expression of TGF-β target genes^[3]. SB-431542 is a selective ALK5 inhibitor with IC50 value of 94nM (measured by GST-ALK5 kinase activity)^[1]. SB-431542 also shows inhibition against ALK4 and ALK7, which are very similar to ALK5 in their kinase domains. Addition of SB-431542 for 24h at a concentration of 10uM can efficiently inhibit the p-Smad2 phosphorylated by activated ALK4, ALK5, and ALK7 in NIH 3T3 cells, with no effect on BMP induced phosphorylation of Smad1, which is mediated by ALKs 2, 3, and 6. The transcription activity mediated by the activated endogenous ALKs 4, 5 and 7 can also inhibited dose-dependently by 0.25, 0.5, 0.75, 1, 2, 5, or 10uM SB-431542^[2]. SB-431542 has performance in both reprogramming and differentiation, as 1. SB-431542 can replace SOX2 in the reprogramming of mouse fibroblasts to iPSCs; 2. Combined with PD0325901 and Thiazovivin, SB-431542 can increase the efficiency of reprogramming human somatic cells to iPSCs; 3. SB-431542, combined with CHIR99021, ISX-9, Forskolin and I-BET151, can direct lineage reprogramming of fibroblasts to mature neurons; 4. SB-431542, in combination with either LDN193189 or Noggin, promotes the differentiation of NPCs from human PSCs; 5. SB-431542 can promote the proliferation and sheet formation of mouse ES-derived endothelial cells; 6. SB-431542 can enhance differentiation of cardiomyocytes.
作用机制SB-431542 acts as a competitive ATP binding site kinase inhibitor^[2].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
C32	10 μM	Function Assay	20h	Inhibits Trypanosoma cruzi Y infection-induced TGFbeta signaling in mink C32 cells at 10 uM	17526757
CHO-HIR	0.01-3 μM	Function Assay	2 h	Inhibits TGFbeta-induced downstream transcriptional activation of ALK5 expressed in CHO-HIR cells assessed as intracellular translocation of EGFP-Smad2 with IC50 of 0.35μM	24055046
H1299	1 μM	Migration Assay	12-24 h	Induces antimigratory activity against human H1299 cells assessed as Inhibition of cell migration with IC50 of 0.5μM	24417479

更多
动物研究
剂量
Mice (i.p.): 4.2 mg/kg^[4], 10 mg/kg^[5]; rat: 2.1 mg/kg^[6] (s.c.)

给药途径
i.p., s.c.
参考文献

动物研究
剂量	Mice (i.p.): 4.2 mg/kg^[4], 10 mg/kg^[5]; rat: 2.1 mg/kg^[6] (s.c.)
给药途径	i.p., s.c.

[1] Callahan JF, Burgess JL, et al. Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5). J Med Chem. 2002 Feb 28;45(5):999-1001.
[2] Halder SK, Beauchamp RD, et al. A specific inhibitor of TGF-beta receptor kinase, SB-431542, as a potent antitumor agent for human cancers. Neoplasia. 2005 May;7(5):509-21.
[3] Colak S, Ten Dijke P, et al. Targeting TGF-β Signaling in Cancer. Trends Cancer. 2017 Jan;3(1):56-71.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6015 mL
- 13.0077 mL
- 26.0154 mL
- 5 mM
- 0.5203 mL
- 2.6015 mL
- 5.2031 mL
- 10 mM
- 0.2602 mL
- 1.3008 mL
- 2.6015 mL

技术信息

CAS号

301836-41-9

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H16N4O3

运输

蓝冰

分子量

384.39

别名

SB-431542

溶解度

DMSO	76.0 mg/mL (197.7 mM)
Water	Insoluble
Ethanol	3.0 mg/mL (7.8 mM)

动物实验配方

2% DMSO+30% PEG 300+water

5 mg/mL

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

C32	10 μM	Function Assay	20h	Inhibits Trypanosoma cruzi Y infection-induced TGFbeta signaling in mink C32 cells at 10 uM	17526757
CHO-HIR	0.01-3 μM	Function Assay	2 h	Inhibits TGFbeta-induced downstream transcriptional activation of ALK5 expressed in CHO-HIR cells assessed as intracellular translocation of EGFP-Smad2 with IC50 of 0.35μM	24055046
H1299	1 μM	Migration Assay	12-24 h	Induces antimigratory activity against human H1299 cells assessed as Inhibition of cell migration with IC50 of 0.5μM	24417479
HaCaT	3.2-50 μM	Function Assay	15 min	Inhibits TGFbeta receptor in human HaCaT cells assessed as Smad phosphorylation with IC50 of 0.172μM	20919678
HaCaT	0.05 μM	Function Assay	2 h	Does not inhibit TGF-beta induced ALK5 activity in HaCaT cells assessed as p3TP-luciferase reporter activity at 0.05 uM	17552507
HEK293T	10 μM	Function Assay	22 h	Inhibits TGBR2 signaling in human HEK293T cells assessed as Inhibition of SMAD activation with IC50 of 0.066μM	23130626
HepG2	-	Function Assay	12 h	Inhibits TGFR-1 in human HepG2 cells expressing PAI-luciferase with IC50 of 0.25μM	19914068
Mouse cardiomyocytes	10 μM	Antimicrobial Assay	4 h	Induces antitrypanosomal activity against Trypanosoma cruzi Y in mouse cardiomyocytes assessed as reduction of intracellular amastigotes at 10 uM	17526757
Mouse cardiomyocytes	10 μM	Antimicrobial Assay	96 h	Induces antitrypanosomal activity against Trypanosoma cruzi Y in mouse cardiomyocytes assessed as Inhibition of trypomastigote release at 10 uM	17526757
Mouse embryo cardiomyocytes	10 μM	Function Assay	1 h	Inhibits invasion of Trypanosoma cruzi Y in mouse embryo cardiomyocytes assessed as pathogen infection at 10 uM	17526757
Mouse embryo cardiomyocytes	10 μM	Function Assay	1 h	Inhibits TGF-beta-1-induced Smad2 phosphorylation in mouse embryo cardiomyocytes at 10 uM	17526757
Mouse embryo cardiomyocytes	10 μM	Function Assay	1 h	Inhibits Trypanosoma cruzi Dm28C infection-induced Smad2 phosphorylation in mouse embryo cardiomyocytes at 10 uM	17526757
Sf9	-	Function Assay	2 h	Inhibits human recombinant ALK5 phosphorylation expressed in Sf9 cells with IC50 of 1.542μM	17552507
Trypanosoma cruzi trypomastigotes	10 μM	Antimicrobial Assay	4 h	Induces antitrypanosomal activity against Trypanosoma cruzi trypomastigotes assessed as effect on parasite morphology at 10 uM	17526757

SB 431542 Catalog No. CSN11900

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